Mycosyst capsules 100 mg 28 pcs
Condition: New product
999 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Fluconazole
Release form
Capsules
Composition
Fluconazole 100 mg; Excipients: colloidal silicon dioxide - 0.6 mg, magnesium stearate - 2.4 mg, talc - 6.6 mg, povidone - 7.2 mg, corn starch - 24.2 mg, lactose (anhydrous) - 99 mg .; The composition of hard gelatin capsules: the lower part - titanium dioxide (CI.I.77891 / E171) - 2%, gelatin - up to 100%; the upper part - indigo carmine (Cw.I.73015 / E132) - 0.0471%, titanium dioxide (Cw.I.77891 / E171) - 4%, gelatin - up to 100%.
Pharmacological effect
Antifungal medication. Fluconazole, a member of the class of triazole antifungal agents, is a selective inhibitor of sterol synthesis in the cell of fungi .; Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit the cytochrome P450 system in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, to a lesser extent, it suppresses the oxidative processes that depend on cytochrome P450 in microsomes of the human liver); Does not possess androgenic activity .; It is active against pathogens of mycoses caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole activity has also been shown in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.
Pharmacokinetics
After oral administration, fluconazole is well absorbed, its bioavailability is 90%. Cmax after ingestion on an empty stomach 150 mg is reached in 0.5-1.5 hours and makes up 90% of the concentration in plasma with a / in a dose of 2.5-3.5 mg / kg. Simultaneous food intake does not affect the absorption of the drug, taken orally .; Distribution; After ingestion and intravenous administration, fluconazole penetrates well into all tissues and body fluids. In the stratum corneum of the epidermis, dermis and sweat fluid, high concentrations are reached that exceed the serum levels. After ingestion of 150 mg on the 7th day, the concentration in the stratum corneum of the skin is 23.4 mcg / g, and 1 week after taking the second dose - 7.1 mcg / kg, the concentration in the nails after 4 months of application at a dose of 150 mg 1 time / week - 4.05 mcg / g in healthy and 1.8 mcg / g in affected nails. Concentrations of the drug in saliva, sputum, breast milk, articular and peritoneal fluid are similar to its concentration in blood plasma. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of the corresponding concentration in plasma.Constant values in the vaginal secretion are reached 8 hours after ingestion and are held at this value for at least 24 hours; Plasma concentrations are directly proportional to dose. 90% equilibrium concentration is achieved by 4-5 days with daily ingestion or in / in the introduction of 1 time / day; Using the dose on the first day, 2 times the usual daily dose, allows you to reach 90% of the equilibrium concentration by the second day. The apparent Vd is close to the total body of water in the body. 11-12% of fluconazole binds to plasma proteins; Metabolism and excretion; It is an inhibitor of CYP2C9 isoenzyme in the liver. No metabolites of fluconazole were detected in the peripheral blood .; T1 / 2 - 30 hours. The pharmacokinetics of fluconazole significantly depends on the functional state of the kidneys, and there is an inverse relationship between T1 / 2 and creatinine clearance. Fluconazole is excreted mainly by the kidneys; however, approximately 80% of the administered dose is excreted unchanged. Fluconazole clearance is directly proportional to creatinine clearance .; After hemodialysis for 3 hours, plasma concentration of fluconazole is reduced by 50%.
Indications
- Cryptococcosis: cryptococcal meningitis, cryptococcal infections of the lungs and skin; cryptococcal sepsis; prevention of recurrence of cryptococcosis in patients with AIDS, organ transplantation or other cases of immunodeficiency; - generalized candidiasis; candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tract), incl. in patients receiving a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis - treatment and prevention; - Candidiasis of the mucous membranes: oral cavity, incl. atrophic candidiasis of the oral cavity associated with the wearing of dentures; pharynx; esophagus and non-invasive bronchopulmonary infections, candiduria; prevention of recurrence of oropharyngeal candidiasis in AIDS patients; - genital candidiasis: vaginal (acute or chronic recurrent); - prevention of fungal infections in patients with malignant tumors that are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy; - mycoses of the skin, trunk, groin area; - deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis and histoplasmosis in patients with normal immunity.
Contraindications
- simultaneous administration of terfenadine (against the background of continuous administration of fluconazole at a dose of 400 mg / day and above) and cisapride, since both drugs prolong the QT interval and increase the risk of developing severe heart rhythm disturbances; - simultaneous use of astemizol; - lactation period (breastfeeding); - lactose intolerance, lactase deficiency, glucose-galactose malabsorption; - Hypersensitivity to the components of the drug or azole compounds with a similar structure .; With caution: liver and / or kidney failure; the appearance of a rash on the background of the use of fluconazole in patients with surface fungal infection and invasive / systemic fungal infections; simultaneous administration of fluconazole with rifabutin or other drugs metabolized by cytochrome P450 isoenzymes; simultaneous administration of terfenadine and fluconazole at a dose of less than 400 mg / day; potentially proarrhythmic states in patients with multiple risk factors (organic heart disease, electrolyte imbalance, simultaneous medication that causes arrhythmias); intolerance to acetylsalicylic acid; pregnancy.
Use during pregnancy and lactation
Use of the drug Mikosist; during pregnancy is possible only when the potential benefit to the mother exceeds the risk to the fetus .; Fluconazole is determined in breast milk in the same concentration as in plasma, so its use during lactation is contraindicated.
Dosage and administration
With cryptococcal infections, the usual dose of fluconazole is 400 mg 1 time / day on the first day of treatment, and then 200-400 mg 1 time / day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological examination, and usually ranges from 6 to 8 weeks .; The recommended duration of treatment for the treatment of cryptococcal meningitis is 10-12 weeks after a negative result of a microbiological study of a sample of cerebrospinal fluid .; To prevent the recurrence of cryptococcal meningitis in AIDS patients after completing the full course of primary therapy, fluconazole is prescribed in a dose of at least 200 mg / day for a long period .; For candidemia, disseminated candidiasis and other invasive candidal infections, the dose of fluconazole is 400 mg on the first day and 200 mg on the following days. If necessary, the dose of the drug can be increased to 400 mg / day.The duration of treatment depends on the clinical efficacy .; In severe systemic candidiasis, it is possible to increase the dose to 800 mg / day. The duration of therapy depends on the clinical effectiveness. It should continue for at least 2 weeks after receiving a negative blood culture or after the disappearance of symptoms of the disease .; When oropharyngeal candidiasis, including patients with impaired immunity, the usual dose of fluconazole is 50-100 mg 1 time / day for 7-14 days. To prevent recurrence of oropharyngeal candidiasis in AIDS patients after completing the full course of primary therapy, 150 mg 1 time per week. If necessary, treatment can be extended, especially in case of severe immunity disorders .; In case of atrophic oral candidiasis associated with wearing dentures, fluconazole is usually prescribed 50 mg 1 time per day for 14 days in combination with antiseptic agents for the treatment of the prosthesis .; For other candidal infections, for example, for esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the daily dose is 50-100 mg for 14-30 days .; In severe mucosal candidiasis - 100-200 mg / day; For the prevention of fungal infections in patients with malignant tumors, the dose of fluconazole is 50 mg 1 time / day as long as the patient is in an increased risk group due to cytostatic or radiation therapy .; With vaginal candidiasis - 150 mg once. To reduce the frequency of relapses, use 150 mg once a month for 4-12 months, sometimes more frequent use may be required .; For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg 1 time / day, depending on the degree of risk of developing a fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or prolonged neutropenia, the recommended dose is 400 mg 1 time / day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after increasing the number of neutrophils more than 1000 / μl, the treatment is continued for another 7 days; With deep endemic mycoses, it may be necessary to use the drug in a dose of 200-400 mg / day for 2 years. The duration of therapy is determined individually; it may be 11–24 months for coccidioidomycosis; 2-17 months for paracoccidioidomycosis and 3-17 months for histoplasmosis .; In children, the drug should not be used in a daily dose in excess of that in adults.The duration of treatment depends on the clinical and mycological effect .; For candidiasis of the mucous membranes, the recommended dose of fluconazole is 3 mg / kg / day. On the first day, a loading dose of 6 mg / kg can be given in order to more quickly reach an equilibrium concentration .; For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg / kg / day, depending on the severity of the disease .; For the prevention of fungal infections in children with reduced immunity, in which the risk of developing an infection is associated with neutropenia, developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg / kg per day, depending on the severity and duration of preservation of induced neutropenia .; In newborns, fluconazole is eliminated more slowly, so in the first 2 weeks of life, the drug is prescribed in the same dose (in mg / kg) as in older children, but with an interval of 72 hours. For children aged 3-4 weeks, the same dose is administered with 48 hour intervals; In elderly patients in the absence of renal dysfunction, the usual recommendations for dosing the drug should be followed. For patients with impaired renal function (CC <50 ml / min), the dosing regimen should be adjusted. Fluconazole is excreted mainly by the kidneys in unchanged form. With a single use of fluconazole dose changes are not required. If necessary, a course of treatment in patients (including children) with impaired renal function should initially enter a loading dose from 50 mg to 400 mg. In the future, the daily dose depending on the evidence is determined by the following table .; > 50 100% 1 time / day; <50 (without dialysis) 50% 1 time / day; Patients on constant dialysis 100% after each dialysis session; Drug administration rules; Enter IV drip at a rate not exceeding 20 mg (10 ml) in min. When translating from a / in the introduction to the reception of capsules and vice versa there is no need to change the daily dose of the drug .; Mikosist; Infusion solution is compatible with the following solutions: 20% glucose solution, Ringer's solution, Hartman solution, potassium chloride solution in glucose, sodium bicarbonate solution, 0.9% sodium chloride solution. Fluconazole infusions can be performed using conventional transfusion kits using one of the solutions listed above.
Side effects
On the part of the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal pain, change in taste, abnormal liver function (hyperbilirubinemia, increased activity of hepatic transaminases, alkaline phosphatase, jaundice, hepatitis, hepatocellular necrosis, including fatal). ; Of the nervous system: headache, dizziness, cramps .; From the side of blood-forming organs: leukopenia, thrombocytopenia, neutropenia, agranulocytosis .; Allergic reactions: skin rash, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, swelling of the face, urticaria, skin itch), bronchial asthma (more often with intolerance to acetylsalicylic acid) .; Since the cardiovascular system: an increase in the duration of the QT interval on the ECG, flickering / fluttering of the ventricles .; Metabolism: hypercholesterolemia, hypertriglyceridemia, hypokalemia .; Other: impaired renal function, alopecia.
Overdose
Symptoms: nausea, vomiting, diarrhea, in severe cases, convulsions, hallucinations, paranoid behavior may occur .; Treatment: gastric lavage, forced diuresis, hemodialysis, symptomatic therapy. After a 3-hour hemodialysis session, the concentration of fluconazole in the blood plasma decreases by approximately 50%.
Interaction with other drugs
In patients receiving fluconazole and indirect anticoagulants of the coumarin series, careful monitoring of the prothrombin time is necessary because it may increase.; Fluconazole, while taking it at the same time, can prolong T1 / 2 sulfonylurea derivatives, therefore, when used together, the possibility of hypoglycemia should be taken into account .; The simultaneous use of fluconazole and phenytoin may be accompanied by an increase in the concentration of phenytoin in a clinically significant degree, which requires a reduction in its dose .; With the simultaneous use of rifampicin and fluconazole decreases Cmax and T1 / 2 of the latter, therefore, if necessary, the combined use should increase the dose of fluconazole .; The combined use of fluconazole and rifabutin is accompanied by an increase in serum concentration of the latter,development of uveitis is possible .; With the combined use of fluconazole and cyclosporine, it is recommended to monitor the concentration of the latter in the blood, since it may increase .; Considering the occurrence of serious life-threatening arrhythmias in patients taking antifungal agents - azole derivatives in combination with terfenadine, their joint administration is contraindicated .; With simultaneous administration of fluconazole and cisapride, cases of adverse reactions of the heart, including paroxysmal ventricular tachycardia, are described. Simultaneous use is contraindicated .; When combined with the use of fluconazole may increase the concentration of zidovudine in the blood plasma. Patients receiving this combination should be monitored to detect side effects of zidovudine .; Reception of fluconazole leads to a decrease in the average rate of clearance of theophylline from blood plasma, therefore, increases the risk of the toxic effect of theophylline and its overdose .; The simultaneous use of fluconazole and midazolam leads to a significant increase in the concentration of the latter in the blood plasma and the risk of developing psychomotor reactions .; At the same time taking fluconazole and hydrochlorothiazide, the concentration of fluconazole in the blood plasma increases by 40% .; At the same time taking fluconazole and tacrolimus, the concentration of the latter in the serum increases, which leads to an increased risk of nephrotoxicity .; Care must be taken when using fluconazole in patients simultaneously receiving other drugs metabolized by cytochrome P450 isoenzymes.
special instructions
Fluconazole treatment should be continued until clinical and hematological remission. Premature discontinuation of treatment leads to relapse .; Since fluconazole is excreted primarily by the kidneys, care should be taken in patients with renal insufficiency. With prolonged treatment with fluconazole, dosing should be carried out taking into account QC .; In rare cases, the use of fluconazole was accompanied by a toxic effect on the liver, including and fatal, mainly in patients with serious concomitant diseases. It is necessary to monitor the function of the liver.If there are signs of liver damage that may be associated with taking fluconazole, the drug should be discontinued .; While taking the drug in patients, there were rare cases of development of exfoliative skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. Patients with AIDS and malignant neoplasms are more likely to develop severe skin reactions with the use of many drugs. When a patient has a superficial rash fungal infection that can be associated with fluconazole, the drug should be discontinued. When rashes appear in patients with invasive / systemic fungal infections, they should be carefully monitored and fluconazole should be canceled when there is a bullous lesion or erythema multiforme .; Care must be taken while taking fluconazole with rifabutin or other drugs metabolized by cytochrome P450 isoenzymes; It is necessary to control the prothrombin time in patients simultaneously receiving fluconazole and indirect anticoagulants coumarin; Impact on the ability to drive vehicles and control mechanisms; Patients should be careful when driving or working with equipment, because during treatment with fluconazole may occur dizziness.